A Readily Applicable Strategy to Convert Peptides to Peptoid-based Therapeutics

作者:Park Minyoung; Wetzler Modi; Jardetzky Theodore S; Barron Annelise E*
来源:PLos One, 2013, 8(3): e58874.
DOI:10.1371/journal.pone.0058874

摘要

Incorporation of unnatural amino acids and peptidomimetic residues into therapeutic peptides is highly efficacious and commonly employed, but generally requires laborious trial-and-error approaches. Previously, we demonstrated that C-20 peptide has the potential to be a potential antiviral agent. Herein we report our attempt to improve the biological properties of this peptide by introducing peptidomimetics. Through combined alanine, proline, and sarcosine scans coupled with a competitive fluorescence polarization assay developed for identifying antiviral peptides, we enabled to pinpoint peptoid-tolerant peptide residues within C-20 peptide. The synergistic benefits of combining these (and other) commonly employed methods could lead to a easily applicable strategy for designing and refining therapeutically-attractive peptidomimetics.

  • 出版日期2013-3-21